Round biconvex tablet of white color, with beveled edges, coated, with a notch on one side, with the engraving "155" on both sides of the risks.
1 coated tablet contains:
Active substance: dydrogesterone - 10 mg.
lactose monohydrate - 111.1 mg,
hypromellose - 2.8 mg,
corn starch - 14.0 mg,
colloidal silicon dioxide - 1.4 mg,
magnesium stearate -0.7 mg.
Shell: Opadri white Y-1-7000 [hypromellose, polyethylene glycol 400, titanium dioxide (E171)] -4.0 mg.
Absorption After oral administration, dydrogesterone is rapidly absorbed. The time to reach the maximum concentration for dydrogesterone varies between 0.5 and 2.5 hours. The absolute bioavailability of dydrogesterone (a dose of 20 mg for oral administration compared with intravenous administration of 7.8 mg) is 28%. Distribution After intravenous administration of dydrogesterone, the volume of distribution in equilibrium is about 1400 liters. More than 90% of didrogesterone and DHD binds to plasma proteins. Metabolism After oral administration, dydrogesterone is rapidly metabolized to DGD. Cmax of the main metabolite of DGD is achieved approximately 1.5 hours after taking the drug. The concentration of DHD in blood plasma is significantly higher than the concentration of dydrogesterone. The ratios of AUC and Cmax of DGD to dydrogesterone are of the order of 40 and 25, respectively. The average elimination half-life of didrogesterone and DHD is from 5 to 7 and from 14 to 17 hours, respectively. A common property of all metabolites is the preservation of the 4,6-diene-3-one configuration of the starting compound and the absence of the 17a-hydroxylation reaction. This explains the lack of estrogen and androgen effects in dydrogesterone. Excretion After ingestion of labeled dydrogesterone, an average of 63% of the dose is excreted through the kidneys (with urine). The total plasma clearance is 6.4 l / min. Dydrogesterone is completely excreted after 72 hours. DGD is found in urine mainly in the form of conjugates of glucuronic acid. The dependence of the pharmacokinetic parameters on the dose and time. The drug is characterized by linear pharmacokinetics with single and multiple oral administration in the dose range from 2.5 mg to 10 mg. When comparing the pharmacokinetic parameters with single and multiple oral administration, it was found that the pharmacokinetics of dydrogesterone and DGD does not change as a result of repeated use. The equilibrium state is reached 3 days after the start of treatment.
In clinical trials, patients who received only dydrogesterone therapy most often encountered: headache / migraine, nausea, menstrual irregularities, tenderness / tenderness of the mammary glands. In clinical studies, as well as during post-marketing applications (spontaneous reports), using only dydrogesterone, the following undesirable effects were observed with the development frequency indicated below (number of reported cases / number of patients): often (> 1/100, <1/10) , infrequently (> 1/1000, <1/100), rarely (> 1/10000, <1/1000). Hematopoietic organs: Rarely: hemolytic anemia. From the central nervous system: Often: headache / migraine. Infrequently: dizziness. Rarely: drowsiness. From the digestive system: Often: nausea. Infrequently: vomiting, impaired liver function (with jaundice, asthenia or malaise, abdominal pain). Allergic reactions: Infrequently: allergic dermatitis (eg, rash, itching, urticaria); Rarely: Quincke's edema, hypersensitivity reactions. From the reproductive system: Often: menstrual irregularities (including metrorrhagia, menorrhagia, oligo- / amenorrhea, dysmenorrhea and irregular menstrual cycles), tenderness / sensitivity of the mammary glands. Rarely: swelling of the mammary glands. From the psyche: Infrequently, depressed mood. Other: Infrequently: weight gain. Rarely: edema, an increase in the size of progestogen-dependent neoplasms (e.g., meningioma). When using certain progestogens in combination with estrogens as part of hormone replacement therapy, the following undesirable effects were noted: breast cancer, endometrial hyperplasia, endometrial cancer, ovarian cancer; venous thromboembolism; myocardial infarction, coronary heart disease, ischemic stroke.